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非小细胞肺癌靶向治疗药物的研究进展
引用本文:赵雷磊,张媛,周金培,张惠斌.非小细胞肺癌靶向治疗药物的研究进展[J].中国药科大学学报,2014,45(2):136-144.
作者姓名:赵雷磊  张媛  周金培  张惠斌
作者单位:中国药科大学新药研究中心;中国药科大学新药研究中心;中国药科大学新药研究中心;中国药科大学新药研究中心
基金项目:国家"重大新药创制"科技重大专项资助项目(No.2013ZX09301303-002)
摘    要:研究发现非小细胞肺癌形成与多种致癌突变密切相关,如表皮生长因子受体(EGFR)突变、间变性淋巴瘤激酶(ALK)重排以及肝细胞生长因子受体(c-MET)扩增等。本文从腺癌和鳞状细胞癌两个亚型的靶向治疗药物入手,分别介绍了非小细胞肺癌潜在的靶点及小分子抑制剂,包括EGFR抑制剂、ALK抑制剂、KRAS抑制剂、c-MET抑制剂、FGFR1抑制剂、PI3K抑制剂、BRAF抑制剂、ERBB2抑制剂以及DDR2抑制剂,为非小细胞肺癌患者临床用药和非小细胞肺癌靶向治疗药物开发提供参考。

关 键 词:非小细胞肺癌  腺癌  鳞状细胞癌  致癌突变  小分子抑制剂  靶向药物

Advances in research on drugs targeting non-small cell lung cancer
ZHAO Leilei,ZHANG Yuan,ZHOU Jinpei and ZHANG Huibin.Advances in research on drugs targeting non-small cell lung cancer[J].Journal of China Pharmaceutical University,2014,45(2):136-144.
Authors:ZHAO Leilei  ZHANG Yuan  ZHOU Jinpei and ZHANG Huibin
Abstract:With the continuous development of molecular biology, people have gained a deeper understanding of non-small cell lung cancer(NSCLC). Researchers have found that multiple oncogenic driver mutations are closely associated with the development, progression and prognosis of NSCLC, such as EGFR mutations, ALK rearrangement, KRAS mutations, c-MET amplification, FGFR1 amplification, PIK3CA mutations, BRAF mutations, ERBB2 amplification, and DDR2 mutation. Adenocarcinoma(ADC)and squamous cell carcinoma(SCC)are two most common subtypes of NSCLC. In this review, we choose targeted therapy drugs of ADC and SCC as an entry point to introduce several potential targets and small molecule inhibitors for the treatment of NSCLC, including EGFR inhibitors, ALK inhibitors, KRAS inhibitors, c-MET inhibitors, FGFR1 inhibitors, PI3K inhibitors, BRAF inhibitors, ERBB2 inhibitors and DDR2 inhibitors. We hope this review will be a helpful guide to clinicians and researchers alike by assisting in therapy decision making and acting as a platform for further study.
Keywords:non-small cell lung cancer  adenocarcinoma  squamous cell carcinoma  oncogenic driver mutation  small molecular inhibitor  targeting drugs
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